反应详情

N-(3-Fluoro-2-(3-fluoropyrrolidin-1-yl)benzylidene)-3,3-dimethylbutan-1-amine (400 mg, 1.359 mmol) was taken in toluene and (S)-2-mercaptosuccinic acid (204.1 mg, 1.359 mmol) was added. The reaction mixture was refluxed overnight with a Dean Stark trap to remove the water. Then the reaction mixture was concentrated, triturated with ether and dried overnight to give crude 2-((5R)-3-(3,3-dimethylbutyl)-2-(3-fluoro-2-((S)-3-fluoropyrrolidin-1-yl)phenyl)-4-oxothiazolidin-5-yl)acetic acid which was used directly in the next step. The product was identified by HPLC and LC/MS. (LC/MS: m/z=427.2 M+1).

1. temperatureThe reaction mixture was refluxed overnight with a Dean Stark trap
2. customto remove the water
3. concentrationThen the reaction mixture was concentrated
4. customtriturated with ether
5. customdried overnight